Method of making liposomes, liposome compositions made by the methods, and methods of using the same

Abstract

A method of preparing liposomes, liposome compositions formed by the process, and methods of using the liposome composition are provided herein.

It is claimed: 
     
       1. A method of making liposomes with an entrapped agent, comprising:
 solubilizing at least about 10 w/w % of vesicle-forming lipids in about 1-12 w/w % of a solvent miscible with water at room temperature to form a lipid solution; 
 separately solubilizing about 2.5-25 w/w % of the agent in about 25-65 w/w % of an aqueous solvent and 0.005-0.01 w/w % of EDTA at room temperature to form an agent containing solution; 
 filtering the agent containing solution; 
 injecting a stream of the lipid solution into the agent containing solution while mixing; and 
 allowing the resulting lipid and agent containing solution to hydrate for at least one hour with frequent mixing; 
 wherein the w/w % is based on the weight of the liposome formulation with the entrapped agent, 
 wherein the resulting liposomes retain at least about 65-100% of the entrapped agent after at least one month storage. 
 
     
     
       2. The method of  claim 1 , wherein the solvent miscible with water comprises an alcohol. 
     
     
       3. The method of  claim 1 , further comprising adding more lipid or a thickener to form a gel after the hydration step. 
     
     
       4. The method of  claim 1 , wherein the vesicle-forming lipids comprises at least about 45-50% phosphatidylcholine. 
     
     
       5. The method of  claim 4 , wherein the phosphatidylcholine is derived from egg or soy. 
     
     
       6. The method of  claims 1 - 4 , wherein the agent is ascorbic acid or a salt thereof. 
     
     
       7. The method of  claim 1 , wherein the agent is glutathione. 
     
     
       8. The method of  claim 1 , wherein the agent is alpha lipoic acid.